CN102579358B - A kind of drug sustained-release pellet and preparation method thereof - Google Patents
A kind of drug sustained-release pellet and preparation method thereof Download PDFInfo
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- CN102579358B CN102579358B CN201110450000.8A CN201110450000A CN102579358B CN 102579358 B CN102579358 B CN 102579358B CN 201110450000 A CN201110450000 A CN 201110450000A CN 102579358 B CN102579358 B CN 102579358B
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Abstract
The present invention relates to slow-release micro-pill changing medicine thing release behavior and preparation method thereof.This slow-release micro-pill includes that, containing the pill heart and sustained-release coating layer, this sustained-release coating layer comprises hydrophobic base and the hydrophilic polymer to pH sensitive.This high molecular polymer in the gastrointestinal tract, has different physical propertys under different pH, and in simple terms, this high molecular polymer can be dissolved in water or the most swelling under the sour environment of stomach, discharges medicine；It is also possible to select different high molecular polymers or the compositions between them, it is allowed in small intestinal or large intestine or rectum be administered, plays the effect of site-specific delivery of drugs.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, specifically refer to slow-release micro-pill changing medicine thing release behavior and preparation method thereof.
Background technology
Micropill refers to that diameter is less than all kinds of pills of 2.5mm, can need to be made into rapid release or slow-release micro-pill according to difference.At present research it is important that slow-release micro-pill, slow-release micro-pill is mixed by medicine with blocker or first makes common capsule core bag release-controlled film the most again and forms.Micropill can tabletted, it is possible to is loaded in capsule by micropill and makes capsule.
Slow-release micro-pill has an advantage that other oral formulations many cannot be compared:
1) big at gastrointestinal tract distribution area, bioavailability is high, and zest is little；
2) little due to particle diameter, affected little (such as pylorus closedown etc.) by the digestive tract conveying food rhythm and pace of moving things；
3) blood drug level can be made to be rapidly reached effective therapeutic concentration, and maintain valid density steady, long, the fluctuation of blood medicine is little；
4) good fluidity of micropill, size is uniform, it is easy to process (such as coating, divided dose)；
5) improve medicine stability, cover disagreeable taste；
6) compatibility of compound preparation it is suitable for；
Although slow-release micro-pill has above-mentioned advantage, but in actual fabrication process, different pharmaceutical is prepared as slow-release micro-pill and will face a different technologies difficult problem.
Summary of the invention
The present invention provides a kind of drug sustained-release pellet, including containing the pill heart and sustained-release coating layer, it is characterised in that this sustained-release coating layer comprises hydrophobic base and the hydrophilic polymer to pH sensitive.This high molecular polymer in the gastrointestinal tract, has different physical propertys under different pH, and in simple terms, this high molecular polymer can be dissolved in water or the most swelling under the sour environment of stomach, discharges medicine；It is also possible to select different high molecular polymers or the compositions between them, it is allowed in small intestinal or large intestine or rectum be administered, plays the effect of site-specific delivery of drugs.Further, described slow releasing preparation so that the pH value of this high molecular polymer generation dissolubility change is between 1-14, preferably between 2-9.Meanwhile, this high molecular polymer can be as slow-release material, i.e. this high molecular polymer can also simplify prescription as the carrier of Drug controlled release simultaneously as the carrier of site-specific delivery of drugs, reduce preparation difficulty, is more easy to the big production of industry.Inventor surprisingly it has been found that, said preparation can be used for preparing the slow release formulation of various medicine, and does not relies on the physicochemical property of medicine.
Further, described hydrophilic polymer molecules amount is more than 6000 so that medicine more preferably discharges, inventor studies discovery, due to micropill small volume, when selecting macromolecule polyalcohol as porogen, medicine can be discharged well, without the incomplete phenomenon of release occurs.
Further, described slow-release micro-pill, prescription calculates according to mass ratio, and Sustained release coating materials weightening finish is the 10%～80% of the ball heart.Generally, the weightening finish of 10%～40% is more particularly suitable, because, the thinnest slow release effect that is not up to, and the thickest drug release that affects, and, when increasing weight bigger, higher molecular weight, the i.e. polymer more than 10000 is used to can obviously improve the incomplete problem of drug release.
Further, described hydrophilic polymer includes but not limited to as alginic acid and salt thereof or chitosan or carbomer or Bo Luobomu.
More even, its pellet core contains hydrophilic back bone material or osmotic pumps penetrating agent.
Inventor provides the second drug sustained-release pellet, and including hydrophobic base, medicine and the hydrophilic polymer to pH sensitive, described hydrophilic polymer includes but not limited to as alginic acid and salt thereof or chitosan or carbomer or Bo Luobomu.Relative to above-mentioned slow-release micro-pill, the second slow-release micro-pill is made without coating.The preparation method of this second slow-release micro-pill, is placed in hydrophobic base, medicine and the hydrophilic polymer to pH sensitive in extrusion spheronization machine, sprays into wetting agent or binding agent, make micropill.
Further, both micropills are pressed into tablet can also mix employing dry mixed with filler and fluidizer after.
Further, above-mentioned slow-release micro-pill can also include that filler is the water-fast compounds such as microcrystalline Cellulose, calcium hydrogen phosphate, calcium carbonate, and above material can be used alone can also be with the use of.
Further, slow release layer also has plasticizer.Plasticizer is further selected from including triethyl citrate, Methyl Benzene-o-dicarboxylate, dibutyl sebacate, diethyl phthalate, dibutyl phthalate.
Inventor it was unexpectedly observed that use micropill rounding prepared by said method, controls power to drug release good, drug release patterns favorable reproducibility by experiment.
Detailed description of the invention
Further describe the present invention by the following examples, it should be noted that these embodiments purpose illustratively provides, and is not meant to limit the scope of the invention.
Embodiment 1 Tamsulosin sustained release pellet and tablet (1000 preparation unit)
Prescription of preparation and preparation method thereof is:
Prescription
The ball heart:
Coating:
Carbomer 8g
Ethyl cellulose 9g
Triethyl citrate 3g
Preparation method:
Take polyvidone and add 80% ethanol dissolving, standby as binding agent；Component in other micropill prescriptions is placed in extrusion spheronization machine, adds adhesive and prepare the ball heart, 60 DEG C of fluid bed dryings；
Taking the ball heart, in putting in coating pan, spray into the coating constituents of acetone solution, be coated, coating is dried 1 hour after terminating.It is dried 12 hours then at 40 DEG C, obtains slow-release micro-pill.
Slow-release micro-pill will be gone to load capsule and get final product.
Or above-mentioned micropill is added microcrystalline Cellulose, magnesium stearate, mixing, it is pressed into sizeable tablet.
Chinese Pharmacopoeia two annex XD the first methods of version in 2010 are used to measure the release of said preparation.
Embodiment 2 Tamsulosin sustained release pellet and tablet (1000 preparation unit)
Prescription of preparation and preparation method thereof is:
Prescription
The ball heart:
Coating:
Sodium alginate 15g
Ethyl cellulose 29g
Magnesium stearate 6g
Preparation method:
Take polyvidone and add 80% ethanol dissolving, standby as binding agent；Component in other micropill prescriptions is placed in extrusion spheronization machine, adds adhesive and prepare the ball heart, 60 DEG C of fluid bed dryings；
Taking the ball heart, in putting in coating pan, spray into the coating constituents of acetone solution, be coated, coating is dried 1 hour after terminating.It is dried 12 hours then at 40 DEG C, obtains slow-release micro-pill.
Slow-release micro-pill will be gone to load capsule and get final product.
Or above-mentioned micropill is added microcrystalline Cellulose, magnesium stearate, mixing, it is pressed into sizeable tablet.
Chinese Pharmacopoeia two annex XD the first methods of version in 2010 are used to measure the release of said preparation.
Embodiment 3 metformin slow-release micro-pill and tablet (1000 preparation unit)
Prescription of preparation and preparation method thereof is:
Prescription
The ball heart:
Coating:
Preparation method:
Take polyvidone and add 80% ethanol dissolving, standby as binding agent；Component in other micropill prescriptions is placed in extrusion spheronization machine, adds adhesive and prepare the ball heart, 60 DEG C of fluid bed dryings；
Taking the ball heart, in putting in coating pan, spray into the coating constituents of acetone solution, be coated, coating is dried 1 hour after terminating.It is dried 12 hours then at 40 DEG C, obtains slow-release micro-pill.
Slow-release micro-pill will be gone to load capsule and get final product.
Or above-mentioned micropill is added microcrystalline Cellulose, magnesium stearate, mixing, it is pressed into sizeable tablet.
Chinese Pharmacopoeia two annex XD the first methods of version in 2010 are used to measure the release of said preparation.
Embodiment 4 metformin slow-release micro-pill and tablet (1000 preparation unit)
Prescription of preparation and preparation method thereof is:
Prescription
The ball heart:
Coating:
Preparation method:
Take polyvidone and add 80% ethanol dissolving, standby as binding agent；Component in other micropill prescriptions is placed in extrusion spheronization machine, adds adhesive and prepare the ball heart, 60 DEG C of fluid bed dryings；
Taking the ball heart, in putting in coating pan, spray into the coating constituents of acetone solution, be coated, coating is dried 1 hour after terminating.It is dried 12 hours then at 40 DEG C, obtains slow-release micro-pill.
Slow-release micro-pill will be gone to load capsule and get final product.
Or above-mentioned micropill is added microcrystalline Cellulose, magnesium stearate, mixing, it is pressed into sizeable tablet.
Chinese Pharmacopoeia two annex XD the first methods of version in 2010 are used to measure the release of said preparation.
Embodiment 5 Tamsulosin sustained release pellet and tablet (1000 preparation unit)
Prescription of preparation and preparation method thereof is:
Prescription
The ball heart:
Coating:
Carbomer 24g
Ethyl cellulose 50g
Triethyl citrate 6g
Preparation method:
Take polyvidone and add 80% ethanol dissolving, standby as binding agent；Component in other micropill prescriptions is placed in extrusion spheronization machine, adds adhesive and prepare the ball heart, 60 DEG C of fluid bed dryings；
Taking the ball heart, in putting in coating pan, spray into the coating constituents of acetone solution, be coated, coating is dried 1 hour after terminating.It is dried 12 hours then at 40 DEG C, obtains slow-release micro-pill.
Slow-release micro-pill will be gone to load capsule and get final product.
Or above-mentioned micropill is added microcrystalline Cellulose, magnesium stearate, mixing, it is pressed into sizeable tablet.
Chinese Pharmacopoeia two annex XD the first methods of version in 2010 are used to measure the release of said preparation.
In addition, it should be noted that measure drug release patterns with capsule during this experimental data and to be prepared as tablet similar, each time point fluctuates without departing from 2%.
Table 1 each embodiment tamsulosin Accumulation dissolution
It should be noted that, above embodiment is just to illustrating the present invention.On the premise of without departing from spirit and substance of the present invention, those skilled in the art can be designed that multiple alternative and the improvement project of the present invention, within it all should be understood to be in protection scope of the present invention.
Claims (2)
1. a metformin slow-release micro-pill, is made up of the ball heart and sustained-release coating layer, it is characterised in that the described ball heart consists of: metformin 250g, microcrystalline Cellulose 35g, lactose 10g, PVPK305g；Described coating consists of: carbomer 8g, sodium alginate 4g, ethyl cellulose 15g, triethyl citrate 3g；Make 1000 preparation unit.
2. a metformin slow-release micro-pill, is made up of the ball heart and sustained-release coating layer, it is characterised in that the described ball heart consists of: metformin 200g, HPMCK100LV35g, microcrystalline Cellulose 60g, PVPK305g；Described coating consists of: chitosan 5g, poloxamer 5g, ethyl cellulose 17g, dimethyl phthalate 3g；Make 1000 preparation unit.
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| CN201110450000.8A CN102579358B (en) | 2011-12-29 | 2011-12-29 | A kind of drug sustained-release pellet and preparation method thereof |
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| CN102579358B true CN102579358B (en) | 2016-08-03 |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101669912A (en) * | 2009-05-25 | 2010-03-17 | 北京诚创康韵医药科技有限公司 | Slow-release composition containing tamsulosin and preparation thereof |
| CN101695478A (en) * | 2009-10-23 | 2010-04-21 | 江苏大学 | Tamsulosin hydrochloride sustained-release pellets and preparation method thereof |
| CN101703511A (en) * | 2009-11-10 | 2010-05-12 | 沈阳药科大学 | Compound tamsulosin and finasteride sustained release capsule and preparation method thereof |
| CN101904818A (en) * | 2009-11-24 | 2010-12-08 | 沈阳药科大学 | Self-assembled composite membrane controlled sustained-release preparation and preparation method thereof |
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Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101669912A (en) * | 2009-05-25 | 2010-03-17 | 北京诚创康韵医药科技有限公司 | Slow-release composition containing tamsulosin and preparation thereof |
| CN101695478A (en) * | 2009-10-23 | 2010-04-21 | 江苏大学 | Tamsulosin hydrochloride sustained-release pellets and preparation method thereof |
| CN101703511A (en) * | 2009-11-10 | 2010-05-12 | 沈阳药科大学 | Compound tamsulosin and finasteride sustained release capsule and preparation method thereof |
| CN101904818A (en) * | 2009-11-24 | 2010-12-08 | 沈阳药科大学 | Self-assembled composite membrane controlled sustained-release preparation and preparation method thereof |
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Address after: 100083 A building, block 15, Tiangong building, No. 30, Haidian District, Beijing, Xueyuan Road Applicant after: COSCI MED-TECH Co.,Ltd. Address before: 100190, room 1410, satellite building, No. 63, Zhichun Road, Beijing, Haidian District Applicant before: COSCI MED-TECH Co.,Ltd. |
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Effective date of registration: 20230323 Address after: 8639, Floor 6, Building 3, No. 3, Yongchang North Road, Daxing District, Beijing, 100176 Patentee after: Beijing Kexin Jurun Pharmaceutical Technology Co.,Ltd. Address before: 100083 15 / F, block a, Tiangong building, 30 Xueyuan Road, Haidian District, Beijing Patentee before: COSCI MED-TECH Co.,Ltd. |